Antiproliferative activities of halogenated thieno[3,2-d]pyrimidines |
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| Affiliation: | 1. Department of Chemistry and Biochemistry, University of Maryland Baltimore County, 1000 Hilltop Circle, Baltimore, MD 21250, USA;2. Department of Biochemistry and Molecular Biology, University of Maryland School of Medicine, 108 N. Greene Street, Baltimore, MD 21201, USA;3. Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium;4. Center for Drug Design, University of Minnesota, 516 Delaware St. SE, Minneapolis, MN 55455, USA;1. Gilead Sciences, 333 Lakeside Drive, Foster City, CA 94404, USA;2. Beryllium, 7869 NE Day Road West, Bainbridge Island, WA 98110, USA;1. Biological Sciences, Sunnybrook Research Institute, 2075 Bayview Avenue, Toronto, ON M4N 3M5, Canada;2. Department of Surgery/Otolaryngology, UCSD School of Medicine, La Jolla, CA 92093, USA;3. Department of Cell Biology and Neuroscience, Nelson Laboratories, Rutgers University, 604 Allison Road, Piscataway, NJ 08854, USA;4. Department of Otolaryngology – Head and Neck Surgery, University of Toronto, Toronto, ON, Canada;5. Department of Laboratory Medicine and Pathobiology, University of Toronto, Toronto, ON, Canada;1. School of Pharmacy, Lanzhou University, Lanzhou 730000, China;2. Experimental Center of Medicine, General Hospital of Lanzhou Military Command, Lanzhou 730050, China;3. Key Laboratory of Stem Cells and Gene Drug of Gansu Province, General Hospital of Lanzhou Military Command, Lanzhou 730050, China;1. University of Chemical Technology and Metallurgy, Department of Organic Synthesis, 8 Kliment Ohridski Blvd., 1756, Sofia, Bulgaria;2. Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, Acad. G. Bonchev Str., Build. 9, 1113, Sofia, Bulgaria;3. Institute of Experimental Morphology, Pathology and Anthropology with Museum, Bulgarian Academy of Science, 1113, Sofia, Bulgaria |
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| Abstract: | The in vitro evaluation of thieno[3,2-d]pyrimidines identified halogenated compounds 1 and 2 with antiproliferative activity against three different cancer cell lines. A structure activity relationship study indicated the necessity of the chlorine at the C4-position for biological activity. The two most active compounds 1 and 2 were found to induce apoptosis in the leukemia L1210 cell line. Additionally, the compounds were screened against a variety of other microbial targets and as a result, selective activity against several fungi was also observed. The synthesis and preliminary biological results are reported herein. |
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| Keywords: | Heterocyclic chemistry Cytostatic Apoptosis Antifungal |
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